Search results for " activity"

H2-Antihistaminika, 32. Mitt. Synthese und H2-antagonistische Wirkung von N-[3-(3-Piperidino-methyl-phenoxy)propyl]-1.3.4-oxadiazol-2-aminen

1986

Es wird uber die Synthese und H2-antagonistische Wirksamkeit von N-[3-(3-Piperidinomethyl-phenoxy)-propyl]-1.3.4-oxadiazol-2-amin und dessen 5-substituierte Derivate berichtet. H2-Antihistaminics, XXXII: Synthesis and H2-Antagonistic Activity of N-[3-(3-(Piperidinomethyl)phenoxy)propyl]- 1.3.4-oxadiazol-2-amines The synthesis and H2-antagonistic activity of N-[3-(3-(piperidinomethyl)phenoxy)propyl]-l.3.4-oxadiazol-2-amine and its 5-substituted derivatives are reported.

Muskelrelaxantien, 4. Mitt. Monoacylbutyroguanamine

1986

Die Umsetzung von Butyroguanamin (1) mit den Carbonsaureanhydriden 2a−f bei 80–120° fuhrt zu den Monoacylbutyroguanaminen 3a−f, deren Struktur durch IR-, 1H-NMR- und MS-Spektren untermauert wird. Unter den hier beschriebenen Verbindungen weisen insbesondere 3e muskelrelaxierende und antidiabetische und 3a trichomonazide und antivirale Wirksamkeit auf, wahrend mit 3b−d herbizide Wirkungen beobachtet werden. Muscle Relaxants, IV: Monoacylbutyroguanamines Reaction of butyroguanamine (1) with the carboxylic acid anhydrides 2a−f at 80–120°C leads to the monoacylbutyroguanamines 3a−f, the structure of which is supported by IR, 1H-NMR, and mass spectra. Among the compounds described here, particul…

Acute prostaglandins and sympathetic activity changes due to amino acids load in essential hypertension

1995

ChemInform Abstract: 1,2,3-Triazole in Heterocyclic Compounds, Endowed with Biological Activity, Through 1,3-Dipolar Cycloadditions

2014

1,3-Dipolar cycloaddition reactions can be considered a powerful synthetic tool in the building of heterocyclic rings, with applications in different fields. In this review we focus on the synthesis of biologically active compounds possessing the 1,2,3-triazole core through 1,3-dipolar cycloaddition reactions. The 1,2,3-triazole skeleton can be present as a single disubstituted ring, as a linker between two molecules, or embedded in a polyheterocycle. The cycloaddition reactions are usually catalysed by copper or ruthenium. Domino reactions can be achieved through dipolarophile anion formation, generally followed by cyclisation. The variety of attainable heterocyclic structures gives an ill…

Effect of Monooxygenase Inducers on the Binding of Benzo-(A)Pyrene Metabolites to Cellular Macromolecules in Perfused Rat Lungs

1978

The irreversible binding of metabolically activated [3H]-benzo(a)pyrene (BP) to cellular macromolecules of isolated perfused rat lungs was studied. Lungs from differently pretreated animals were perfused in situ in a recirculating system without ventilation. BP with a specific activity of 10 mCi/μmol was added to 50 ml perfusion medium containing 40% washed bovine erythrocytes to a final concentration of 1 μM. DNA, RNA and protein fractions were isolated and assayed for irreversibly bound radioactivity.

Antimykotische Wirkstoffe, 16. Mitt. Halogenierte Cyanaminomethylenpiperidine und -piperazine

1984

Die in Gegenwart der sekundaren Amine 5a-e mit Hilfe von s-Triazin (2) als Dreikomponentenreaktion durchgefuhrte Aminomethinylierung von Cyanamid (1) liefert die korrespondierenden als Dehydro-N-Mannich-Basen aufzufassenden Cyanaminomethylenheterocyclen 6a-e. Insbesondere 6a und 6e besitzen antimykotische Wirksamkeit. Antimycotic Agents, XVI: Halogenated (Cyanaminomethylene)piperidines and -piperazines The aminomethinylation of cyanamide (1) by means of s-triazine (2), carried out as three-component reaction in the presence of the secondary amines 5a–e, yields the cyanaminomethylene heterocycles 6a–e, which are to be classed as dehydro-N-Mannich bases. Compounds 6a and 6e in particular show…

Light Regulation of the Thylakoid LHCII Protein Phosphorylation at the Substrate Level

1998

The distribution of light energy between the two photosystems as well as the light-induced turnover of PSII proteins are regulated by the reversible phosphorylation of LHCII and the PSII-core proteins. The thylakoid protein kinase(s) is activated by a signal transduction system involving the interaction of reduced plastoquinone with the quinol oxidation site of the cytochrome bf complex [1]. Phosphorylation of the mobile pool of LHCII induces dissociation of this antenna from PSII and allows its interaction with the PSI in the stroma exposed membranes (state transition)[21. Dephosphorylation of LHCII by a membrane -bound phosphatase appears to be regulated by a cyclophilinlike protein locat…

Antibakterielle Wirkstoffe, 6. Mitt.1) 2,4-Unsymmetrisch dialkylierte Pyrimido[1,2-a]benzimidazole

1982

Durch Kondensation von 2-Aminobenzimidazol (1) mit 2,4-Hexandion (2a) entsteht das Isomerenpaar 3a/3b, mit 6-Methyl-2,4-heptandion (2b) das Isomerengemisch 3c/3d, wahrend mit 1-Phenyl-2,4-pentandion (2c) die Isomere 3e und 3f gebildet werden. Die Trennung der Isomere ist durch Saulenchromatographie, die Strukturfestlegung auf spektroskopischem Wege, moglich. 2-Imino-2H-s-triazino[2,1-b]benzoxazol weist antibakterielle Wirksamkeit auf. Antibacterial Drugs, VI: 2,4-Unsymmetrically Dialkylated Pyrimido[1,2-α]benzimidazoles Condensation of 2-aminobenzimidazole (1) with 2,4-hexanedione (2a) leads to the pair of isomers 3a/3b. Condensation with 6-methyl-2,4-heptanedione (2b) yields the isomers 3c…

H2-Antihistaminika, 25. Mitt. Synthese und H2-antagonistische Wirkung monosubstituierter 1,2,4-Oxadiazol-3,5-diamine

1985

Es wurden die N3- bzw. N5-substituierten 1,2,4-Oxadiazol-3,5-diamine 4a-e und 5a-e dargestellt und auf Histamin-H2-antagonistische Aktivitat untersucht. H2-Antihistaminics, XXV: Synthesis and H2-Antagonistic Activity of Monosubstituted 1,2,4-Oxadiazole-3,5-diamines The N3-or N5-substituted 1,2,4-Oxadiazole-3,5-diamines 4a-e and 5a-e were prepared and tested for histamine H2-antagonistic activity.

Adult Lactose Tolerance Is Not an Advantageous Evolutionary Trait

2004

To the Editor. I read with great interest the recent article from Fomon1 in which he refers to the well-known hypothesis that views the variable frequencies of lactase persistence in different human populations and, consequently, the possibility for some adults to feed on milk (lactose tolerance) as an advantageous evolutionary trait that has been genetically determined and brought about through centuries of natural selection. This notion stands as a common statement in current medical literature, and most authors have accepted its validity since the 1970s.2,3 Because adult mammals are lactose-intolerant, this hypothesis is, moreover, based on the low percentage of lactose malabsorption and…